SPEN-IN-1

• CAT Number: I042377
• CAS Number: 2863686-82-0
• Molecular Formula: C27H20N4O
• Molecular Weight: 416.47
• Purity: ≥95%

SPEN-IN-1 (compound X1) is an inhibitor of SPEN which is a protein factor with a Kd value of 47 nM. SPEN-IN-1 has high selectivity for RepA, a 431-nucleotide domain in Xist (a non-coding RNA prototype) that comprises 8.5 units of a GC-rich motif responsible for gene silencing[1].
SPEN-IN-1 (0-100 μM) inhibits RepA-PRC2 and RepA-SPEN interactions with IC50 values of 30 and 48 µM, respectively[1].
SPEN-IN-1 inhibits RepA, PRC2 and SPEN with Kd values of 400, 47 and 420 nM, respecctively[1].
SPEN-IN-1 selectively disrupts the interactions of Xist with cognate proteins in vitro and inside cells[1].
SPEN-IN-1 strongly inhibits H3K27me3 and PRC2 accumulation[1].
SPEN-IN-1 reduces RepA-SPEN interaction in vivo[1].

Reference

[1]. Aguilar R, et al. Targeting Xist with compounds that disrupt RNA structure and X inactivation. Nature. 2022 Apr;604(7904):160-166.
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